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Drugs Targeting TGF-β Induced Plasticity

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Sendurai Mani, PhD

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Description: Three therapeutic mechanisms for inhibiting the TGF-β pathway in cancer: Galunisertib inhibits TGFβ-RI kinase activity, preventing Smad2/3 activation. It has been combined with sorafenib, radiation, gemcitabine, and temozolomide. Fresolimumab acts as a TGF-β trap by competitively binding TGF-β and has been combined with radiation in clinical trials. Bintrafusp-alfa is a first-in-class dual inhibitor of PD-L1 and TGF-β. Adapted from Fig. 7, Proactive and reactive roles of TGF-β in cancer.

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Three therapeutic mechanisms for inhibiting the TGF-β pathway in cancer: Galunisertib inhibits TGFβ-RI kinase activity, preventing Smad2/3 activation. It has been combined with sorafenib, radiation, gemcitabine, and temozolomide. Fresolimumab acts as a TGF-β trap by competitively binding TGF-β and has been combined with radiation in clinical trials. Bintrafusp-alfa is a first-in-class dual inhibitor of PD-L1 and TGF-β. Adapted from Fig. 7, Proactive and reactive roles of TGF-β in cancer.

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